IS2980B - Methods for Preparation of 4 - [[4 - [[4- (2-cyanoethyl) -2,6-dimethylphenyl] amino] -2-pyrimidinyl] amino] benzonitrile - Google Patents

Methods for Preparation of 4 - [[4 - [[4- (2-cyanoethyl) -2,6-dimethylphenyl] amino] -2-pyrimidinyl] amino] benzonitrile

Info

Publication number
IS2980B
IS2980B IS7621A IS7621A IS2980B IS 2980 B IS2980 B IS 2980B IS 7621 A IS7621 A IS 7621A IS 7621 A IS7621 A IS 7621A IS 2980 B IS2980 B IS 2980B
Authority
IS
Iceland
Prior art keywords
amino
cyanoethyl
benzonitrile
dimethylphenyl
pyrimidinyl
Prior art date
Application number
IS7621A
Other languages
Icelandic (is)
Other versions
IS7621A (en
Inventor
Philippe Robert Schils Didier
Josephus Maria Willems Joannes
Petrus Anna Maria Jozef Medaer Bart
Therese Jeanne Pasquier Elisabeth
Adriaan Jan Janssen Paul
Heeres Jan
Gerardus George Leenders Ruben
Emile Georges Guillemont Jérome
Original Assignee
Janssen Pharmaceutica N.V.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=31725448&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=IS2980(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Janssen Pharmaceutica N.V. filed Critical Janssen Pharmaceutica N.V.
Publication of IS7621A publication Critical patent/IS7621A/en
Publication of IS2980B publication Critical patent/IS2980B/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C253/00—Preparation of carboxylic acid nitriles
    • C07C253/20—Preparation of carboxylic acid nitriles by dehydration of carboxylic acid amides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C253/00—Preparation of carboxylic acid nitriles
    • C07C253/30—Preparation of carboxylic acid nitriles by reactions not involving the formation of cyano groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Oncology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
IS7621A 2002-08-09 2004-12-29 Methods for Preparation of 4 - [[4 - [[4- (2-cyanoethyl) -2,6-dimethylphenyl] amino] -2-pyrimidinyl] amino] benzonitrile IS2980B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP02078306 2002-08-09
PCT/EP2003/050366 WO2004016581A1 (en) 2002-08-09 2003-08-07 Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile

Publications (2)

Publication Number Publication Date
IS7621A IS7621A (en) 2004-12-29
IS2980B true IS2980B (en) 2017-09-15

Family

ID=31725448

Family Applications (1)

Application Number Title Priority Date Filing Date
IS7621A IS2980B (en) 2002-08-09 2004-12-29 Methods for Preparation of 4 - [[4 - [[4- (2-cyanoethyl) -2,6-dimethylphenyl] amino] -2-pyrimidinyl] amino] benzonitrile

Country Status (26)

Country Link
US (3) US7399856B2 (en)
EP (1) EP1529032B1 (en)
JP (1) JP4822707B2 (en)
KR (2) KR101140785B1 (en)
CN (4) CN100554245C (en)
AR (1) AR040964A1 (en)
AU (1) AU2003266413B2 (en)
CA (2) CA2493794C (en)
CL (1) CL2010000284A1 (en)
CY (1) CY1114428T1 (en)
DK (1) DK1529032T3 (en)
EA (1) EA007953B1 (en)
ES (1) ES2422196T3 (en)
HK (4) HK1081527A1 (en)
HR (1) HRP20050104B1 (en)
IL (1) IL166710A (en)
IS (1) IS2980B (en)
MX (1) MXPA05001541A (en)
MY (1) MY144894A (en)
NO (1) NO330013B1 (en)
NZ (1) NZ538611A (en)
PL (1) PL208533B1 (en)
PT (1) PT1529032E (en)
SI (1) SI1529032T1 (en)
TW (1) TWI314146B (en)
WO (1) WO2004016581A1 (en)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7638522B2 (en) * 2001-08-13 2009-12-29 Janssen Pharmaceutica N.V. Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino] benzonitrile
MY169670A (en) 2003-09-03 2019-05-08 Tibotec Pharm Ltd Combinations of a pyrimidine containing nnrti with rt inhibitors
JO3429B1 (en) 2001-08-13 2019-10-20 Janssen Pharmaceutica Nv Hiv inhibiting pyrimidines derivatives
US8101629B2 (en) * 2001-08-13 2012-01-24 Janssen Pharmaceutica N.V. Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile
EP1529032B1 (en) * 2002-08-09 2013-04-24 Janssen Pharmaceutica NV Processes for the preparation of 4- 4- 4-(2 -cyanoethenyl)-2,6-dimethylphenyl )amino) -2-pyrimidinyl)amino benzonitrile
US7504410B2 (en) * 2002-11-28 2009-03-17 Schering Aktiengesellschaft Chk-, Pdk- and Akt-inhibitory pyrimidines, their production and use as pharmaceutical agents
WO2005123662A1 (en) * 2004-06-18 2005-12-29 Janssen Pharmaceutica N.V. Modified heck reaction
JP4922937B2 (en) * 2004-09-02 2012-04-25 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 4-((4-((4- (2-cyanoethenyl) -2,6-dimethylphenyl) amino) -2-pyrimidinyl) amino) benzonitrile fumarate
AU2005279157B2 (en) * 2004-09-02 2011-07-14 Janssen Pharmaceutica N.V. Fumarate of 4-[[4-[[4- (2-cyanoethenyl) -2,6-dimethylphenyl]amino)-2-pyrimidinyl)amino]benzonitrile
RS51923B2 (en) * 2004-09-02 2022-05-31 Janssen Pharmaceutica Nv Salt of [[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyi]amino]-2-, pyrimidinyl]amino]benzonitrile
CA2577288C (en) * 2004-09-02 2010-11-30 Janssen Pharmaceutica N.V. Hydrochloride of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile
AP2296A (en) * 2004-09-02 2011-10-31 Janssen Pharmaceutica Nv Hydrochloride of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile.
US7314962B2 (en) * 2005-04-15 2008-01-01 E. I. Du Pont De Nemours & Co. Alkylation of aromatic compounds
EP1888537B1 (en) * 2005-05-26 2013-09-11 Janssen R&D Ireland Process for preparing 4-[(1,6-dihydro-6-oxo-2-pyrimidinyl)amino benzonitrile
CL2008000746A1 (en) 2007-03-14 2008-09-22 Tibotec Pharm Ltd PHARMACEUTICAL COMPOSITION IN SOLUTION INCLUDING TMC278 AND A WATER SOLUBLE POLYMER; PREPARATION PROCESS OF SUCH COMPOSITION; AND USE OF A POWDER UNDERSTANDING TMC278 TO TREAT AIDS.
AU2008274185B2 (en) * 2007-07-12 2014-07-03 Janssen Sciences Ireland Uc Crystalline form of (E) 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2 pyrimidinyl]amino]benzonitrile
WO2012125993A1 (en) 2011-03-17 2012-09-20 Teva Pharmaceutical Industries Ltd. Solid state forms of rilpivirine base, and rilipivirine salts
AP2013006779A0 (en) * 2011-04-15 2013-03-31 Emcure Pharmaceuticals Ltd An improved rilpivirine process
EP2702044B1 (en) 2011-04-25 2017-03-22 Hetero Research Foundation Process for rilpivirine
CA2848631C (en) 2011-09-16 2019-10-01 Hetero Research Foundation Rilpivirine hydrochloride
WO2013170421A1 (en) * 2012-05-14 2013-11-21 上海迪赛诺药业有限公司 Rilpivirine hydrochloride alcoholate polymorph and preparation method thereof
WO2013179105A1 (en) * 2012-06-01 2013-12-05 Laurus Labs Private Limited Improved process for preparation of rilpivirine and pharmaceutically acceptable salts thereof
WO2014009968A2 (en) * 2012-07-12 2014-01-16 Hetero Research Foundation Process for rilpivirine using novel intermediate
CZ201532A3 (en) 2015-01-21 2015-02-25 Zentiva, K.S. Process for preparing extremely pure rilpivirine and salt thereof
CN106008366A (en) * 2016-05-25 2016-10-12 山东大学 Preparation method of rilpivirine
BR112019007564A2 (en) 2016-10-24 2019-07-02 Janssen Sciences Ireland Unlimited Company dispersible compositions
EP3870568B1 (en) 2018-10-25 2023-06-28 Minakem Process for the preparation of rilpivirine
CN110526873B (en) * 2019-08-15 2022-09-16 复旦大学 Cyanovinyl substituted benzodiarylpyrimidine compound and preparation method and application thereof
US11166952B2 (en) 2019-11-29 2021-11-09 Aptorum Therapeutics Limited Composition including rilpivirine and method for treating tumors or cancer
CN112010810B (en) * 2020-09-09 2024-01-30 瑞阳制药股份有限公司 Method for preparing high-purity rilpivirine intermediate by one-pot method
CN112778214A (en) * 2021-01-13 2021-05-11 安徽贝克联合制药有限公司 Intermediate for synthesizing rilpivirine, synthesis method thereof and rilpivirine synthesis method

Family Cites Families (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3459731A (en) 1966-12-16 1969-08-05 Corn Products Co Cyclodextrin polyethers and their production
EP0002341B1 (en) 1977-11-28 1982-01-20 Barry Boettcher Complexes of bivalent copper, methods of preparation thereof and compositions containing said complexes
US5691364A (en) 1995-03-10 1997-11-25 Berlex Laboratories, Inc. Benzamidine derivatives and their use as anti-coagulants
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
IL123654A (en) 1995-11-23 2001-08-08 Janssen Pharmaceutica Nv Process for preparing solid mixtures of cyclodextrins, and pharmaceutical compositions comprising such solid mixtures
GB9705361D0 (en) 1997-03-14 1997-04-30 Celltech Therapeutics Ltd Chemical compounds
US6982091B2 (en) 2001-08-29 2006-01-03 Umd, Inc. Vaginal delivery of chemotherapeutic agents and inhibitors of membrane efflux systems for cancer therapy
AP1468A (en) 1998-03-27 2005-09-23 Janssen Pharmaceutica Nv Hiv inhibiting pyrimidine derivatives.
DE69943247D1 (en) 1998-03-27 2011-04-14 Janssen Pharmaceutica Nv HIV-inhibiting pyrimidine derivatives
JP2000035628A (en) 1998-07-16 2000-02-02 Konica Corp Silver halide photographic sensitive material
AU5438299A (en) 1998-08-29 2000-03-21 Astrazeneca Ab Pyrimidine compounds
SK287269B6 (en) 1998-11-10 2010-05-07 Janssen Pharmaceutica N. V. Pyrimidine derivative, its use, process for its preparation and pharmaceutical composition, combination and product containing thereof
BR0008804A (en) 1999-03-09 2002-04-16 Upjohn Co 4-oxo-4, 7-dihydrothieno [2,3-b] pyridine-5-carboxamides as antiviral agents
CZ302788B6 (en) 1999-04-15 2011-11-09 Bristol-Myers Squibb Company ?N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolcarboxamide, use thereof and pharmaceutical composition in which it is comprised
GB9914258D0 (en) 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
SK285240B6 (en) 1999-09-24 2006-09-07 Janssen Pharmaceutica N. V. Antiviral formulations
DE19945982A1 (en) 1999-09-24 2001-03-29 Knoll Ag Velocity-determined particles
KR20030024659A (en) 2000-02-17 2003-03-26 암겐 인코포레이티드 Kinase Inhibitors
GB0004888D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004887D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
ES2542326T3 (en) * 2000-05-08 2015-08-04 Janssen Pharmaceutica Nv HIV replication inhibitors
US6596729B2 (en) * 2000-07-20 2003-07-22 Bristol-Myers Squibb Company Tricyclic-2-pyridone compounds useful as HIV reverse transcriptase inhibitors
WO2002070470A2 (en) 2001-03-02 2002-09-12 Smithkline Beecham Corporation Benzophenones as inhibitors of reverse transcriptase
EP1373257B9 (en) 2001-03-29 2008-10-15 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
MY169670A (en) 2003-09-03 2019-05-08 Tibotec Pharm Ltd Combinations of a pyrimidine containing nnrti with rt inhibitors
JO3429B1 (en) * 2001-08-13 2019-10-20 Janssen Pharmaceutica Nv Hiv inhibiting pyrimidines derivatives
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
CN1290893C (en) 2002-05-03 2006-12-20 詹森药业有限公司 Polymeric microemulsions
EP1529032B1 (en) 2002-08-09 2013-04-24 Janssen Pharmaceutica NV Processes for the preparation of 4- 4- 4-(2 -cyanoethenyl)-2,6-dimethylphenyl )amino) -2-pyrimidinyl)amino benzonitrile
WO2004050068A1 (en) 2002-11-29 2004-06-17 Janssen Pharmaceutica N.V. Pharmaceutical compositions comprising a basic respectively acidic drug compound, a surfactant and a physiologically tolerable water-soluble acid respectively base

Also Published As

Publication number Publication date
CN102702111A (en) 2012-10-03
HK1174922A1 (en) 2013-06-21
US7399856B2 (en) 2008-07-15
BR0313545B1 (en) 2021-07-27
WO2004016581A1 (en) 2004-02-26
HK1081527A1 (en) 2006-05-19
TW200418810A (en) 2004-10-01
CL2010000284A1 (en) 2010-08-20
DK1529032T3 (en) 2013-07-08
PL373679A1 (en) 2005-09-05
TWI314146B (en) 2009-09-01
CN102702111B (en) 2014-12-17
PT1529032E (en) 2013-07-11
EP1529032A1 (en) 2005-05-11
AR040964A1 (en) 2005-04-27
US20080167464A1 (en) 2008-07-10
JP4822707B2 (en) 2011-11-24
HK1161869A1 (en) 2012-08-10
CN101481356A (en) 2009-07-15
US20060167253A1 (en) 2006-07-27
CA2493794C (en) 2010-05-25
KR101086678B1 (en) 2011-11-25
CN101481356B (en) 2012-07-11
NO20050524L (en) 2005-02-01
US7705148B2 (en) 2010-04-27
KR101140785B1 (en) 2012-05-03
US20070191407A1 (en) 2007-08-16
US7563922B2 (en) 2009-07-21
IL166710A (en) 2010-12-30
NO330013B1 (en) 2011-02-07
MY144894A (en) 2011-11-30
EA007953B1 (en) 2007-02-27
KR20050040906A (en) 2005-05-03
EA200500325A1 (en) 2005-06-30
IL166710A0 (en) 2006-01-15
MXPA05001541A (en) 2005-04-19
PL208533B1 (en) 2011-05-31
AU2003266413A1 (en) 2004-03-03
HK1129671A1 (en) 2009-12-04
CA2686429C (en) 2010-11-16
CN102225902B (en) 2013-04-24
HRP20050104A2 (en) 2006-03-31
SI1529032T1 (en) 2013-08-30
NZ538611A (en) 2007-03-30
HRP20050104B1 (en) 2014-02-14
CN100554245C (en) 2009-10-28
KR20100127889A (en) 2010-12-06
BR0313545A (en) 2005-07-12
ES2422196T3 (en) 2013-09-09
CA2493794A1 (en) 2004-02-26
EP1529032B1 (en) 2013-04-24
CN102225902A (en) 2011-10-26
CY1114428T1 (en) 2016-08-31
JP2005537303A (en) 2005-12-08
IS7621A (en) 2004-12-29
AU2003266413B2 (en) 2009-04-02
CA2686429A1 (en) 2004-02-26
CN1681774A (en) 2005-10-12

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